SIRT6 activator 12q 是有效的、选择性的和具有口服活性的SIRT6激活剂，对 SIRT1、SIRT2、SIRT3、SIRT5、SIRT6 的IC50值分别为 171.20、>200、>200、>200、0.58 μM。SIRT6 activator 12q 抑制细胞生长和迁移。SIRT6 activator 12q 诱导细胞凋亡 (Apoptosis) 和细胞周期停滞在 G2 期。SIRT6 activator 12q 显示出抗癌活性。
| 生物活性 | SIRT6 activator12q is potent, selective and orally activeSIRT6activator withIC50values of 171.20, >200, >200, >200, 0.58 μM forSIRT1,SIRT2,SIRT3,SIRT5,SIRT6, respectively.SIRT6 activator12q inhibits cell growth and migration.SIRT6 activator12q inducesApoptosisand cell cycle arrest at G2 phase.SIRT6 activator12q shows anticancer activity[1]. |
| IC50& Target | SIRT1 171.2 μM (IC50) | SIRT2 >200 μM (IC50) | SIRT3 >200 μM (IC50) | SIRT5 >200 μM (IC50) | SIRT6 0.58 μM (IC50) |
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体外研究
(In Vitro) | SIRT6 activator 12q (2.5, 5, 10 μM; 14, 18 days) 以剂量依赖性方式抑制 PANC-1、BXPC-3、MIAPaCa-2 和 AsPC-1 细胞的集落形成[1].
SIRT6 activator 12q (10, 25, 50 μM; 48 h) 以剂量依赖性方式诱导细胞凋亡和细胞周期停滞在 G2 期[1]。
SIRT6 activator 12q (12.5, 25, 50 μM; 48 h) 以剂量依赖性方式降低 PANC-1 和 BXPC-3 细胞中 H3K9ac、H3K18ac 和 H3K56ac 的蛋白表达[1]。
Cell Viability Assay[1] | Cell Line: | PANC-1, BXPC-3, MIAPaCa-2, and AsPC-1 cells | | Concentration: | 0-100 μM | | Incubation Time: | 72 h | | Result: | Showed antiproliferative activity with IC50s of 4.43, 8.27, 7.10, 9.66 μM for PANC-1, BXPC-3, MIAPaCa-2, and AsPC-1 cells, respectively. |
Cell Cycle Analysis[1] | Cell Line: | PANC-1, BXPC-3 cells | | Concentration: | 10, 25, 50 μM | | Incubation Time: | 48 h | | Result: | Induced cell cycle arrest at G2 phase in a dose-dependent manner. |
Apoptosis Analysis[1] | Cell Line: | PANC-1, BXPC-3 cells | | Concentration: | 10, 25, 50 μM | | Incubation Time: | 48 h | | Result: | Induced apoptosis by increased Annexin V+ populations in a concentration-dependent manner. |
Western Blot Analysis[1] | Cell Line: | PANC-1, BXPC-3 cells | | Concentration: | 12.5, 25, 50 μM | | Incubation Time: | 72 h | | Result: | Decreased the protein levels of H3K9ac, H3K18ac, and H3K56ac in PANC-1 and BXPC-3 cells in a dose-dependent manner. |
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体内研究
(In Vivo) | SIRT6 activator 12q (100, 150 mg/kg; p.o.; daily for 30 days) 以剂量依赖性方式抑制小鼠肿瘤生长[1]。
| Animal Model: | BALB/c female nude mice (human pancreatic tumor xenograft model of PANC-1)[1] | | Dosage: | 100, 150 mg/kg | | Administration: | P.o.; daily for 30 days | | Result: | Inhibited tumer growth in a dose-dependent manner, and a tumor inhibition rate of 90.25% at a dose of 150 mg/kg. |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | Please store the product under the recommended conditions in the Certificate of Analysis. |
